A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods...A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods. Crystal structure of one new compound was also reported. The pharmacological properties, including antibacterial(14 bacterial species), antifungal(7 strains), antimalarial, anti-trypanosomal and anti-HIV activities of the compounds, were investigated. Cytotoxicity of the tested compounds was evaluated against human cervix adernocarcinoma cells(He La). Bacterial minimum inhibitory concentration(MIC) results by broth microdilution method showed that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoc and Klebsiella pneumonia were more sensitive in the presence of tested compounds with an MIC value of 15.6 μg/m L. All the tested compounds showed good to moderate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with a minimum cell death concentration(MFC) of 15.6 μg/m L. Compound 1 showed greater antimalarial and anti-trypanosomal properties with very low to no cytotoxic effects against He La cells as compared with compound 5, while other compounds exhibited poor activity. Compounds 1–5 demonstrated good activity against HIV type-1. These Schiff base compounds could be used as good antimicrobial agents.展开更多
Four novel Schiff bases were synthesized by the condensation reaction of 2-hydroxyl-3-nitrobenzaldehyde with either benzothiazoles or benzimidazolamines. The compounds 1–4 were characterized by spectroscopic and anal...Four novel Schiff bases were synthesized by the condensation reaction of 2-hydroxyl-3-nitrobenzaldehyde with either benzothiazoles or benzimidazolamines. The compounds 1–4 were characterized by spectroscopic and analytical methods. The crystal structures of 6-methoxy-1,3-benzothiazol-2-amine and compound 2 are reported only. The 6-methoxy-1,3-benzothiazol-2-amine was found to crystallize in the orthorhombic crystal system in the space group Pbca, having eight molecules in the unit cell, while compound 2 was found to crystallize in the monoclinic crystal system in the space group P2_1/c. The biological activities of these compounds were investigated by evaluating their antibacterial, antifungal, antimalarial, anti-HIV and anti-trypanosomiasis activities. These compounds displayed very interesting antibacterial, antifungal, antimalarial, anti-trypanosomiasis, anti-HIV and low cytotoxicity activity against HeLa cells.展开更多
文摘A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods. Crystal structure of one new compound was also reported. The pharmacological properties, including antibacterial(14 bacterial species), antifungal(7 strains), antimalarial, anti-trypanosomal and anti-HIV activities of the compounds, were investigated. Cytotoxicity of the tested compounds was evaluated against human cervix adernocarcinoma cells(He La). Bacterial minimum inhibitory concentration(MIC) results by broth microdilution method showed that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoc and Klebsiella pneumonia were more sensitive in the presence of tested compounds with an MIC value of 15.6 μg/m L. All the tested compounds showed good to moderate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with a minimum cell death concentration(MFC) of 15.6 μg/m L. Compound 1 showed greater antimalarial and anti-trypanosomal properties with very low to no cytotoxic effects against He La cells as compared with compound 5, while other compounds exhibited poor activity. Compounds 1–5 demonstrated good activity against HIV type-1. These Schiff base compounds could be used as good antimicrobial agents.
基金the Faculty of Science, Department of Applied Chemistry, University of Johannesburg for financial support and its facilities for this projectsupported by the South African Medical Research Council(MRC) with funds from the National Treasury under its Economic Competitiveness and Support Package+3 种基金Rhodes University “Sandisa Imbewu”supported by the Alexander von Humboldt FoundationTWAS (The World Academy of Sciences)the National Research Foundation (NRF) for funding
文摘Four novel Schiff bases were synthesized by the condensation reaction of 2-hydroxyl-3-nitrobenzaldehyde with either benzothiazoles or benzimidazolamines. The compounds 1–4 were characterized by spectroscopic and analytical methods. The crystal structures of 6-methoxy-1,3-benzothiazol-2-amine and compound 2 are reported only. The 6-methoxy-1,3-benzothiazol-2-amine was found to crystallize in the orthorhombic crystal system in the space group Pbca, having eight molecules in the unit cell, while compound 2 was found to crystallize in the monoclinic crystal system in the space group P2_1/c. The biological activities of these compounds were investigated by evaluating their antibacterial, antifungal, antimalarial, anti-HIV and anti-trypanosomiasis activities. These compounds displayed very interesting antibacterial, antifungal, antimalarial, anti-trypanosomiasis, anti-HIV and low cytotoxicity activity against HeLa cells.
